ES2390282T3 - Oregano compositions for oral care and their methods of use - Google Patents

Abstract

An oral care composition in the form of a dentifrice comprising an active ingredient comprising a safe and effective amount of one or more active compounds of an oregano extract, wherein at least one of the one or more active compounds of the oregano extract is selected from carvacrol, thymol and rosmarinic acid, an anti-tartar system comprising as active ingredients to control tartar from 0.5 to 1.5% by weight tetrasodium pyrophosphate, from 1 to 10% by weight sodium tripolyphosphate and 0, 5 to 1.5% by weight of a copolymer of maleic anhydride and methyl vinyl ether, amounts in% by weight based on the weight of the composition, and an orally acceptable carrier.

Description

Oregano compositions for oral care and their methods of use.

Background of the Invention

Human periodontal diseases are inflammatory disorders that are the result of complex interactions between periodontopathogens and the host's immune response. It is believed that there are two interrelated aspects for the progression of periodontal disease, the first is the activation of the host's immune system and the second is the production of oxygen radicals and their related metabolites. The increased production of oxygen radicals can contribute to oxidative stress, which is believed to be involved in periodontal disease.

Gingivitis is the inflammation or infection of the gums and alveolar bones that support the teeth. It is generally believed that gingivitis is caused by mouth bacteria (especially bacteria that promote plaque formation) and toxins formed as bacteria byproducts. It is believed that plaque and bacterial toxins promote inflammation of oral tissue inside the mouth. Periodontitis is a state of disease with progressive worsening compared to gingivitis, where the gums become inflamed and begin to recede from the teeth and recess cavities form, which can ultimately result in the destruction of bone and bone. periodontal ligament Thus, chronic infection and inflammation potentially result in subsequent loss of teeth. Additionally, inflammation of the oral tissue can be caused by surgery, localized injury, trauma, or necrosis, or various systemic origins.

It is generally believed that the cellular components involved in these diseases and conditions include epithelial tissue, gingival fibroblasts, and circulating leukocytes, all of which contribute to the host's response to pathogenic factors generated by bacteria. Thus, bacterial infection increases the host's immune response and decreases the healing process by generating free radical species (reactive oxygen species) and regulates upward inflammatory mediators that cause significant tissue damage.

Free radicals are atoms, ions or molecules that contain an unpaired electron, and as such are generally unstable and show a short half-life. Reactive oxygen species (ERO) are produced during various biochemical processes, and include superoxide anions (O2), hydrogen peroxide (H2O2), hydroxyl radicals (OH), and non-radical oxidants such as singlet oxygen (1O2) . ERO formation can occur as part of many cellular processes including mitochondrial respiration, immune cell responses, cell injury, heat, radiation of many origins, from the metabolism of drugs and other chemicals. EROs are highly reactive and modify important cell macromolecules. EROs initiate or accelerate disease processes.

In one example, EROs are generated during inflammation by phagocytic leukocytes, such as activated neutrophils that produce an "oxidative burst" of superoxide radicals, which are believed to be an essential factor in producing the cytotoxic effect of activated neutrophils. In addition, superoxides can be produced by physiologically endothelial cells by reaction with nitric oxide, a physiological regulator, forming peroxynitrite, ONOO- which can deteriorate and give rise to hydroxyl radicals, OH. Other sources of oxiradicales are the "losses" of electrons from mitochondrial electron transport chains or the interrupted endoplasmic reticulum, prostaglandin synthesis, catecholamine oxidation, and platelet activation.

EROs are believed to participate in almost all disease processes and aging processes. It is believed that the increased formation of ROS in pathological conditions causes cellular lesions through the action of these highly reactive molecules by cross-linking proteins, DNA mutagenesis, and peroxidant lipids.

Another aspect of the immune response is the production of various intra- and inter-cellular mediators of inflammation. A class of mediators studied extensively for their effect on the inflammatory response are arachidonic acid metabolites, namely prostaglandins and leukotrienes, which are produced through the enzymatic pathways of cyclooxygenase or lipoxygenase. These metabolites have been implicated as major mediators in gingivitis, periodontitis, osteomyelitis and other inflammatory diseases.

It would be desirable to have a method of treating a mammalian subject that has an infection, inflammation, and potential cellular lesion in the oral tissue, destroying the etiological pathogens of the infection, reducing the production of one or more inflammation mediators, and reducing the Free radical reactive oxygen species to reduce cellular tissue lesions to promote healing.

Brief summary of the invention

The present invention provides a composition for oral care according to claim 1.

The present invention therefore provides an antibacterial, anti-inflammatory, and antioxidant active ingredient for oral care.

The composition can be used to reduce inflammation of the oral tissue in the oral cavity.

The oral care composition of the present invention can be used in a method to provide one

or more oral health benefits to an oral cavity of a mammalian subject. The method comprises preparing an oral care composition comprising an orally acceptable carrier; and a safe and effective amount of an active ingredient comprising one or more active compounds of an oregano extract, the compounds being selected from carvacrol, thymol and rosmarinic acid. The oral composition is contacted as prepared with one or more oral surfaces of the oral cavity to provide the benefits thereto.

It has been found that the compositions and methods of this invention provide advantages over the antibacterial and antiplaque compositions of the prior art, by providing an oral care composition to promote multiple benefits for oral care in a single active ingredient. The active ingredient comprises one or more active compounds of an oregano extract, the compounds being selected from carvacrol, thymol and rosmarinic acid. The active ingredient is highly effective against gram-positive and gram-negative bacteria involved in various diseases and diseases of the oral cavity. In addition, the oral care composition provides anti-inflammatory and antioxidant effects to the oral cavity to promote healing and to reduce tissue damage and aging. Additionally, the oral composition comprises an active ingredient that is natural and is derived from a botanical source. Other uses, benefits and embodiments of the present invention are apparent from the description set forth herein.

Detailed description of the invention

In accordance with an embodiment of the present invention, a very effective antimicrobial, antioxidant, anti-inflammatory oral composition is provided having a combination of one or more active compounds isolated from an oregano extract, the compounds being selected from carvacrol, thymol and acid Rosmarinic

The oral compositions of the present invention inhibit the growth of various oral bacteria that are involved in plaque formation and that cause oral diseases. The oral composition of the present invention is applied to one or more oral surfaces of the oral cavity, and promotes general oral health, including inhibition of plaque formation, gingivitis, periodontitis, halitosis, and the like. For example, in one embodiment of the present invention, where an oral care composition comprises an orally acceptable release carrier and a safe and effective amount of oregano extract, the compounds being selected from carvacrol, thymol and rosmarinic acid, observed that oregano extract has anti-inflammatory activity, antioxidant activity, and is highly effective against both gram-positive and gram-negative anaerobic bacteria, including those that form plaque and cause halitosis. Thus, the oral compositions of the present invention provide multiple benefits for oral care simultaneously.

An additional advantage of the present invention is that the antibacterial active ingredients of various embodiments of the oral care composition are derived from botanical ingredients that have been used as food for thousands of years. Such extracts are suitable as ingredients for daily use with an oral hygiene care product, such as toothpaste.

The compositions of the present invention comprise at least one active compound found in an oregano extract, the compounds being selected from carvacrol, thymol and rosmarinic acid. As contemplated herein, such "oregano extract" is an extract obtained from dried leaves, cortex (ie bark), root, stem, flower, or any suitable part of a plant of the Lamiaceae family, preferably of the genus Origanum. For example, suitable extracts include those of Origanum vulgare (commonly known as "oregano", "wild oregano", or "wild marjoram"), including its sub-species (Origanum vulgare ssp.), Origanum onites (commonly known as " Italian oregano "or" Turkish oregano "), Origanum majorana (commonly known as" marjoram "or" sweet marjoram ") and Origanum heracleoticum. Origanum vulgare subspecies includes O. vulgare ssp. vulgare, O. vulgare ssp. viride, and O. vulgare ssp. hirtum (commonly known as "Greek oregano" or "wild oregano"). As referred to below, "oregano" encompasses all suitable species and subspecies of the genus Origanum. The term "extract" also encompasses synthetic or semi-synthetic equivalents of such a natural extract or one of its active components. In certain embodiments of the present invention, the active ingredient in the oral composition comprises one or more active compounds, the compounds being selected from carvacrol, thymol and rosmarinic acid, which have been isolated from an oregano extract that includes said one or more active compounds In other embodiments, the active ingredient comprises a complete oregano extract. It should be noted that certain oregano extracts are in lipophilic carriers, such as the case of essential oils, or when the extract is diluted in an oily carrier. Other extracts may be partially or completely separated from lipophilic carriers and contain only the active compounds of the extract and hydrophobic carriers or solvents. The extracts may be in liquid or dry powder forms. The terms "oregano extract" (which includes an extract form and at least one active compound) and one or more active compounds of an oregano extract are used interchangeably herein.

In one embodiment, the oregano extract is obtained from dried oregano leaves prepared by extracting the plant material using an appropriate solvent. Preferred solvents include methanol, ethanol, methylene chloride, hexane, cyclohexane, pentane, petroleum ether, chloroform, ethylene dichloride, and hydrofluoroalkanes, such as 1,1,1,2-tetrafluoroethane (HFA-13A). Generally, a part of the plant tissue (on a dry basis) is extracted with 5 to 50 parts, preferably 15 parts to 30 parts of solvent using an extraction apparatus in which the solvent is contacted with the plant material for obtaining a concentrated paste which is then subjected to one or more additional extraction steps with different solvents to further concentrate the paste originally obtained for a prolonged period of time, preferably from 6 hours to 1-2 days, more preferably for about 1 day .

Other extraction methods include steam distillation or extraction with supercritical fluids. In one embodiment of the present invention, oregano extract is isolated by extraction with supercritical fluid (SFE) using carbon dioxide (CO2). Thus, according to the present invention, oregano or active oregano compounds are extracted from the oregano plant by any of a variety of suitable extraction methods known to one skilled in the art. It is said that oregano contains more than 30 compounds, such as carvacrol, thymol and rosmarinic acid.

Although not limited to any theory to which the present invention is linked, carvacrol and thymol are believed to provide the antimicrobial properties of oregano extracts and rosmarinic acid provides anti-oxidant properties. However, as described above, more than thirty active compounds have been identified in oregano extract, which represent a broad complement of compounds that contribute to efficacy in a variety of areas and functionality. The oral compositions of the present invention comprising an active ingredient of oregano extract are also effective as anti-inflammatory agents.

The "Inflammation" of the oral tissue generally refers to a localized protective response caused by tissue injury or destruction, which serves to destroy, dilute or sequester both the damaging agent and the injured tissue. In the acute form, it is characterized by pain, heat, redness, swelling, and loss of function. Chronic inflammation is a slow process and characterized mainly by the formation of new connective tissue. Chronic inflammation is often a continuation of acute inflammation or a form of prolonged low-grade inflammation (such as that associated with periodontitis or gingivitis) and usually causes permanent tissue damage. Histologically, inflammation involves a complex series of events, including dilation of the arterioles, capillaries and venules, with increased permeability and blood flow; exudation of fluids, including plasma proteins, and leukocyte migration in the inflammatory locus. The inflammation corresponds to improved levels of pro-inflammatory cell mediators, or substances that are released by the cells, for example, as a result of the interaction of an antigen with an antibody or by the action of an antigen with a sensitized lymphocyte.

In the practice of the invention, the oral composition comprising said one or more active ingredients of oregano are applied to the sites of inflamed oral tissue at a concentration that reduces the production of one or more inflammatory cell mediators. In various embodiments of the present invention, the anti-inflammatory active ingredient of the oral composition simultaneously inhibits the action and / or formation of multiple proinflammatory mediators, for example, both PGE2 and TNF-a. Each respective mediator generally has a different mechanism in the pathogenesis of a disease.

In various embodiments, the oral compositions comprise oregano extract, containing said active ingredient or said active ingredients at a concentration in which the production of one or more proinflammatory mediators, such as, for example, PGE2 decreases significantly. However, as recognized by those skilled in the art, a complete suppression of the formation of these cell mediators is also potentially detrimental to the mammalian subject, and in accordance with certain embodiments of the present invention, the production of cytokines is not entirely repressed Thus, in various embodiments, oregano extract is present in the oral composition at a concentration that prevents the expression in excess of one or more inflammatory mediators (which prevents an intrinsic mechanism for chronic disease), but still allows a production enough of certain desirable mediating molecules (which are pleiotropic) to maintain homeostasis and normal cellular functions at baseline levels.

In various embodiments, oregano extract or one or more of its active compounds are used to prepare oral compositions, in the form of dentifrices. The concentration of the active ingredient that contains at least one active compound derived from an oregano extract depends on the relative concentration of the active compounds present in the extract, or the purity of the compounds and, as such, it is contemplated that the amount of extract of oregano or active compounds present can be varied as recognized by those skilled in the art.

In one embodiment, an oral composition comprises a safe and effective amount of an active ingredient in an amount of 0.0001 to 10% by weight. In certain embodiments, the active ingredient is present in the oral composition at a concentration of 0.001 to 5%. In other embodiments, the active ingredient is present from 0.01 to 3%.

In various embodiments, an active ingredient comprising oregano, thereby providing the active compounds, is present in the oral composition. As described above, the active ingredient comprises one or more active compounds isolated from an oregano extract, as in other embodiments where the active ingredient contains the oregano extract or a derivative thereof that includes the one or more active ingredients. In one embodiment, an oral composition comprises an active ingredient that has one or more active compounds (which may include embodiments in which the compound or active compounds are contained in an oregano extract) present in the oral composition at a concentration of 0.001 at 3% by weight, more preferably from 0.01 to 3%. In another embodiment, the one or more active compounds comprise less than 1% of the oral composition, and in certain embodiments they are between 0.001 and 1% by weight. In other embodiments, the one or more active compounds comprise between 0.01 and 1% of the oral composition, and in other embodiments 0.1 to 0.5% of the oral composition.

In certain embodiments, the present invention provides multiple oral care benefits for oral care to a mammalian subject and there may not be a need for additional active ingredients. In one such embodiment, an oral care composition comprises an active ingredient consisting essentially of one

or more active compounds of an oregano extract. In another embodiment, an oral care composition comprises an active ingredient consisting essentially of an oregano extract, thereby providing the active compounds.

The oral care composition of the invention comprises an anti-tartar system. In certain embodiments, an oral care composition of the present invention has an additional active agent ingredient in addition to the one or more active compounds of an oregano extract. Additional active ingredients should not react with or impair the efficacy and bioavailability of oregano extract or any other ingredient in the composition, thus maintaining a stable and effective oral composition.

An optional active substance is applicable for the prevention or treatment of a hard or soft tissue condition or disorder of the oral cavity, the prevention or treatment of a physiological disorder or condition, or to provide a cosmetic benefit. In various embodiments, the active component is an "active component for oral care" applicable to treat or prevent a disorder or provide a cosmetic benefit within the oral cavity (eg, to teeth, gum or other hard or soft tissue of the oral cavity). In other embodiments, the active component is a "systemic active component," which is applicable to treat or prevent a disorder that, in whole or in part, is not a disorder of the oral cavity. Thus, the compositions of the present invention can also be used for the treatment or prevention of systemic disorders, such as the improvement of global systemic health characterized by a reduction in the risk of development of systemic diseases, such as cardiovascular disease. , stroke, diabetes, severe respiratory infection, premature and low birth weight infants (including dysfunction of neurological / developmental function associated with postpartum), and the associated increased risk of mortality.

Optional active components for oral care among those useful herein include bleaching agents, anticaries, periodontal active substances, abrasives, breath fresheners, odor control agents, tooth desensitizers, salivary stimulants, non-stick agents , plate dispersing agents, and combinations thereof. It is understood that while the general attributes of each of the above categories of active components may differ, there may be some common attributes and any given material may serve multiple purposes within two or more such categories of active components.

In various embodiments, a highly effective anti-plate, antibacterial, and anti-inflammatory oral care composition contains an active ingredient comprising one or more active compounds of an oregano extract. However, in certain embodiments of the present invention, an additional antimicrobial / antibacterial ingredient may be included in the oral care compositions. If added, the anti-plate active ingredients (for example, antibacterials) should not react with or impair the efficacy and bioavailability of oregano extract.

Antibacterial agents suitable for use in addition to the oregano extract used in the present invention include other known antibacterial botanical extracts or active compounds isolated from such extracts. Non-limiting examples of natural antibacterial extracts include those isolated from green tea or oolong tea, cúcuta, cranberries and other plants of the Ericaceae family, honeysuckle, grape seeds, myrobalan, rosemary, East Indian nut, neem , niruri, and pine bark.

Green tea and oolong tea are isolated from Camellia sinensis. The active components are believed to be polyphenolic catechins including catechin, epocatechin, epigallocatechin, epicatechin gallate, gallocatechin and epigallocatechin. Cuscuta extracts are obtained from one or more of the following families of Annonaceae, Berberidaceae, Menispenmaceae, Papaveraceae, Ranunculaceae, Rutaceae, Zingiberaceae, Nadina, Mahonia, Thalictrum spp. It is believed that the active compound is berberine. Honeysuckle extracts (Lonicera caprifolium) are obtained from the flower of the honeysuckle plant. The active polyphenolic substances in honeysuckle extract are believed to be chlorogenic acid and / or lutenoline flavonoids. The Ericaceae family generally refers to more than 100 genera and the more than 4,000 associated species, such as those described in US Patent No. 5,980,869 to Sanker, et al. In certain embodiments, extracts of plants of the genus Vaccinium are useful as natural antibacterial extracts, such as cranberry (Vaccinium macrocarpon).

Other natural extracts that are known antimicrobial agents are those contained in the International Cosmetic Ingredient Dictionary and Handbook, tenth ed., 2004, including the following extracts. The grape seed is extracted from Vitis Vinifera seed. Mirobalán is preferably extracted from the fruit of Terminalla bellerica. Rosmarinus officinalis leaf is isolated to create rosemary extract. The pine bark extract is preferably extracted from the cortex (bark) of Pinus pinaster (Maritime Pine). The leaf of the East Indian nut (Albizia lebbek) is used for the extract. The extract of the bark of the neem or loamy plant (Melia azadirachta) is a known antibacterial component. Niruri extract or Phyllanthus niruri is also a known antibacterial extract.

Extracts suitable for use in the present invention can be obtained from any part of the plant including leaf, stem, bark, pulp, seed, meat, juice, root and mixtures thereof. It is preferred that the extract be obtained from the leaf, pulp and seed, more preferably from the leaf, the flower or the bark. Natural extracts containing antibacterial active compounds that are useful as additional antiplate agents, for example, antibacterial agents, in oral compositions must be safe and suitable for use in mammals.

Other useful antimicrobial agents include nonionic and anionic agents known to one skilled in the art. Examples of non-ionic agents include substantially non-cationic water-insoluble antibacterial agents. For example, said antibacterial agents include an alkylphenoxyphenol; a cycloalkylphenoxyphenol; a 9,10-dihydrophenanthrenol; an alkylphenol, a cycloalkylphenol; a phenolic compound; a halogenated carbanilide; a halogenated salicylanilide; a benzoic ester; a halogenated diphenyl ether, and mixtures thereof.

The alkylphenoxyphenol or cycloalkyl-phenoxyphenol or 9,10-dihydrofenantrenol non-ionic antibacterial includes a non-cationic antibacterial phenol containing, with respect to the hydroxyl group, an alkyl or cycloalkyl group, preferably tert-butyl (t-butyl), in the 2 , and substituents in one or both of positions 4 and 5, one of which may be phenyl or alkyl- or cycloalkyl-phenyl substituted at positions 2 ', 3' and / or 4 ', preferably 4'-t-butyl-phenyl or a phenanthrene containing a hydroxyl substituent in the 2 or 3 position and alkyl or cycloalkyl substituents, preferably t-butyl, in the other of the 2 and 3 positions and in at least one of the other rings and are described in US Pat. United States No. 5,723,500 to Stringer et al., issued March 3, 1998.

The water-insoluble non-ionic alkylphenol or cycloalkylphenol includes a phenol containing, with respect to the hydroxyl group, an alkyl or cycloalkyl group, preferably tert-butyl (t-butyl), in position 2, and substituents in one or both of positions 4 and 5, one or both of which may be alkyl or cycloalkyl, one of which is preferably t-butyl, such as those described in United States Patent No. 5,912,274, Stringer et al., 15 June 1999

Phenolic compounds among those useful herein include phenol and its homologs, monohalophenols and polyalkylphenophenols and aromatic halophenols, resorcinol and its derivatives, and bisphenolic compounds, such as those described in US Patent No. 5,368,844, Gaffar et al., issued on November 29, 1994. Certain preferred phenolic compounds are n-hexylresorcinol and 2,2'-methylene-bis (4-chloro-6-bromophenol).

Halogenated carbanilides, halogenated salicylanilides and illustrative benzoic esters are described in US Patent No. 5,776,435, Gaffar et al., Issued July 7, 1998. Halogenated carbanilides include 3,4,4'-trichlorocarbanilide , 3-trifluoromethyl-4,4'-dichlorocarbanilide, and 3,3 ', 4-trichlorocarbanilide. Halogenated salicylanilides include 4'5-dibromosalicylanilide, 3,4 ', 5-trichlorosalcylanilide, 3,4', 5-tribromosalicylanilide, 2,3,3 ', 5-tetrachlorosalicylanilide, 3,3', 5-tetrachlorosalicylanilide, 3,5- dibromo-3'-trifluoromethylsalicylanilide, 5-n-octanoyl-3'trifluoromethyl-salicylanilide, 3,5-dibromo-4'-trifluoromethylsalicylanilide, 3,5-dibromo-3'-trifluoromethylsalicylanilide (Fluorphene), and mixtures thereof. The benzoyl esters include methyl-p-hydroxybenzoic ester, ethyl phydroxybenzoic ester, propyl-p-hydroxybenzoic ester, and butyl-p-hydroxybenzoic ester.

A particularly suitable non-ionic antiplate antibacterial agent is a diphenyl ether selected from the group comprising 2,4,4'-trichloro-2'-hydroxy diphenyl ether (triclosan) and 2,2'-dihydroxy-5,5'-dibromodiphenyl ether. Triclosan is particularly suitable for use as an additional antiplate antibacterial agent.

In various embodiments, additional antiplate antibacterial agents added to the oral composition of the present invention comprise from 0.0001% to 10%, preferably from 0.001% to 5%, more preferably from 0.01% to 3%, depending on the concentration of active compounds and the form of the oral composition.

The oral composition of the present invention may contain an anticaries agent, such as a source of fluoride ions or a fluorine-providing component. In various embodiments, the fluoride-based anticaries agent is present in an amount sufficient to deliver 25 ppm to 5,000 ppm fluoride ions. Useful anticaries agents include inorganic fluoride salts, such as soluble alkali metal salts. For example, the preferred fluoride sources useful in the oral composition are sodium fluoride, potassium fluoride, sodium fluorosilicate, ammonium fluorosilicate, sodium monfluorophosphate (MFP), and amine fluorides, including Olaflur (N'octadecyltrimethylenediamine-N , N, N'-tris (2-ethanol) -dihydrofluoride). Tin compounds, including those based on stannous fluoride and stannous chloride are also useful herein. In certain embodiments, sodium fluoride, sodium MFP, or Olaflur (N'-octadecyltrimethylenediamine-N, N, N'-tris (2-ethanol) -dihydrofluoride) is preferred as an anticaries ingredient.

Where sodium fluoride is the only fluoride-releasing salt present, an amount of 0.01% to 5%, 0.05% to 1% or 0.1% to 0.5%, by weight is illustratively present of sodium fluoride in the composition.

In various embodiments, the oral compositions of the present invention comprise antisarro agents to prevent and / or minimize stone formation. One or more such agents may be present.

The anti-scale system includes tetrasodium pyrophosphate (TSPP) and sodium tripolyphosphate (STPP). Phosphate and polyphosphate salts are generally used in the form of their water-soluble cationic species totally or partially neutralized (for example, potassium, sodium or ammonium salts, and any of their mixtures).

The composition of the present invention includes an anti-calculation system further comprising a linear synthetic anionic polycarboxylate polymer. Synthetic anionic polycarboxylates are used in the dentifrice compositions of the present invention as an agent for improving the efficacy of tartar control agents, as well as for a variety of other active ingredients. The linear anionic polycarboxylate is preferably a 1: 4 to 4: 1 copolymer of maleic anhydride-methyl vinyl ether (methoxyethylene), which preferably has a molecular weight (MW) of about 30,000 to about 2,500,000. These copolymers are commercially available, for example, as Gantrez® AN-139 (PM 1,000,000), AN-119 (PM 200,000) and Solution S-97 (PM 1,500,000), from ISP Corporation.

The antisarro active ingredient system of the oral care composition comprises TSPP of 0.5 to 1.5% by weight, STPP of 1 to 10% by weight, and a copolymer of maleic anhydride and methylvinyl ether of 0.5 to 1 , 5% by weight.

In another embodiment, the oral composition comprises a stannous ion source acceptable orally, useful, for example, to help reduce gingivitis, plaque, calculus, caries or sensitivity. One or more of these sources may be present. Suitable sources of stannous fluoride ions include, without limitation stannous fluoride, other stannous halides such as stannous chloride dihydrate, stannous pyrophosphate, salts of organic stannous carboxylates, such as formate, acetate, gluconate, lactate, tartrate, oxalate, malonate and citrate stannous, ethylene glyoxide stannous and the like. One or more sources of stannous ion are optionally and illustratively present in a total amount of 0.001% to 10%, for example 0.1% to 7% or 1% to 5% by weight of the composition.

In another embodiment, the oral composition comprises a source of orally acceptable zinc ions useful, for example, as an antimicrobial agent, anti-calculus or to freshen breath. One or more of these sources may be present. Suitable zinc ion sources include without limitation zinc acetate, zinc citrate, zinc gluconate, zinc glycinate, zinc oxide, zinc sulfate, sodium zinc citrate and the like. One or more sources of zinc ions are optionally and illustratively present in a total amount of 0.001% to 3%, for example 0.1% to 1%, by weight of the composition.

In another embodiment, the composition comprises an orally acceptable sialagogue (saliva stimulating agent) useful for example in improving dry mouth. One or more such agents may be present in a total effective amount of saliva stimulator. Suitable psychologists include without limitation food acids such as citric, lactic, malic, succinic, ascorbic, adipic, fumaric and tartaric acid.

In another embodiment, the composition comprises an oral breath freshener acceptable. One or more such agents may be present in a total amount effective to freshen the breath. Suitable breath freshening agents include without limitation zinc salts such as zinc gluconate, zinc citrate and zinc chlorite, a-ionone and the like.

In addition to the antibacterial agents described above, which are optionally added to the oral compositions of the present invention, and preferably prevent plaque formation, another embodiment of the composition comprises an orally acceptable antiplate agent. An anti-plate agent can work by an anti-adhesion mechanism, plate interrupting mechanism, or both. One or more such agents may be present in a total effective amount antiplate. Other suitable antiplate agents include, without limitation, stannous, copper, magnesium and strontium salts, dimethicone copolyols such as cetyl dimethicone copolyol, papain, glucoamylase, glucose oxidase, urea, calcium lactate, calcium glycerophosphate, strontium polyacrylates and agents chelants such as citric and tartaric acids and alkali metal salts thereof.

In another embodiment, the composition comprises an orally acceptable anti-inflammatory agent other than the oregano compounds described above. One or more such agents may be present in a total effective anti-inflammatory amount. Suitable anti-inflammatory agents include, without limitation steroidal agents such as flucinolone and hydrocortisone, and non-steroidal agents (NTHE) such as ketorolac, flurbiprofen, ibuprofen, naproxen, indomethicine, diclofenac, etodolac, indomethacin, sulindac, tolmetine, ketoprofenophene , piroxicam, nabumetone, aspirin, diflunisal, meclofenamate, mefenamic acid, oxyphebutazone and phenylbutazone. One or more anti-inflammatory agents are optionally present in the composition in an effective anti-inflammatory amount.

In various embodiments, the orally acceptable dentifrice vehicle used to prepare an oral composition comprises an aqueous phase. As those skilled in the art recognize, the oral compositions of the present invention optionally include other materials, such as, for example, viscosity modifiers, diluents, surfactants, such as surfactants, emulsifiers, and foam modulators, pH modification, abrasives, humectants, emollients and moisturizers, agents to impart a sensation in the mouth, sweetening agents, flavoring agents, colors, preservatives and combinations thereof. It is understood that while the general attributes of each of the above categories of materials may differ, there may be some common attributes and any given material may serve multiple purposes within two or more of such material categories. Preferably, said carrier materials are selected for compatibility with the active ingredient comprising an oregano extract, as well as with other ingredients of the composition.

The composition of the present invention can be used in a method to promote oral health in an oral cavity and for the treatment of plaque on a buccal surface (tooth surface) of a mammalian subject. In one embodiment, a method of providing one or more oral health benefits to an oral cavity of a mammalian subject involves the preparation of an oral care composition comprising an orally acceptable carrier and a safe and effective amount of a active ingredient comprising one or more active compounds, selected from carvacrol, thymol and rosmarinic acid, from an oregano extract. The prepared oral composition is contacted with an oral surface of the oral cavity. The oral composition of the present invention containing the active ingredient comprising an oregano extract provides multiple benefits for oral health including antigingivitis, anti-periodontitis, anti-inflammatory, anti-aging, breath freshener, and combinations thereof. For example, in certain embodiments of the present invention, contacting the oral composition with the oral surface reduces inflammation of the oral tissue. This anti-inflammatory effect can occur due to the antioxidant properties of oregano extract that is believed to prevent damage induced by oxiradicales by capturing free radical compounds (ERO) after they have formed in the oral cavity; reducing one or more mediators of inflammation in the inflamed tissue in the oral cavity, or by both mechanisms. The present invention also provides an antimicrobial effect when the oral composition comprising oregano extract containing the active compounds is contacted with an oral surface. The active ingredient comprising an oregano extract is effective against Gram negative and Gram positive oral bacteria, both of which are involved in halitosis, plaque formation, and chronic oral diseases, such as gingivitis and periodontitis. Therefore, the present invention is an effective antibacterial agent.

Additionally, the contact of the oral tissue with the oral composition comprising an oregano extract, which contains the active compounds, serves to reduce or improve one or more conditions selected from the group consisting of: plaque formation, halitosis, gingivitis and periodontitis.

The oral care composition is prepared in the form of a toothpaste. The oral composition is preferably in contact with or is applied regularly to an oral surface, preferably with a daily schedule, at least once a day for several days, but alternatively, every two or three days. More preferably, the oral composition is applied to the oral surfaces 1 to 3 times a day, at a pH of about 4.5 to about 10, generally about 5.5 to about 8, preferably about 6 to 8, during at least 2 weeks up to 8 weeks or more until a lifetime.

The oral compositions of the present invention can be prepared by properly mixing the ingredients. Dentifrices are prepared by adding various salts (including fluoride) and sweeteners (for example, saccharin) to the water, where they are mixed. In another container, all humectants, gums and polymers are added together. The aqueous mixture described above is added to the container with the humectants, gums and polymers. The combined ingredients are optionally heated from 60 to 71 ° C (140 ° to 160 ° F) to disperse the gums and polymers. The heated mixture is then cooled to less than about 38 ° C (100 ° F). The mixture is then combined with abrasives, when mixed at high speed under vacuum for 15 to 20 minutes. The aromatic oil (and / or alcohol) and the active ingredient are then added to the mixture and mixed at high speed and under vacuum until it is sufficiently dispersed. The surfactant or surfactants are added and the mixture is mixed again to disperse it.

The following examples further illustrate the present invention, but it is understood that the invention is not limited thereto. All amounts and proportions referred to herein and in the appended claims are by weight unless otherwise indicated.

Example I

A dentifrice formulation is prepared containing a powdered extract of the active ingredient of oregano extracted from Origanum vulgare available from Cedarville provided at 0.3%. In addition, additional active ingredients were added to control tartar containing tetrasodium pyrophosphate (TSPP), sodium tripolyphosphate (STPP). A copolymer of maleic anhydride and methyl vinyl ether (GANTREZ ® S97 liquid) was also added with the ingredients listed in Table I.

A dentifrice composition having the ingredients listed in Table I is prepared by the following method. They are dispersed in sodium saccharin water, sodium monofluorophosphate, tetrasodium pyrophosphate (TSPP), sodium tripolyphosphate (STPP) and any other salts and mixed in a conventional mixer with stirring. The humectants, p. ex. Glycerin and sorbitol are added to the aqueous mixture with stirring. Next, organic thickeners, such as carrageenan, and any polymers, such as GANTREZ®, are added. The resulting mixture is stirred and heated from about 60 to 71 ° C (140 ° to 160 ° F), until a homogeneous gel phase is formed, and then cooled. A pigment such as TiO2, dye, and any acid or base (for example, NaOH) required to adjust the pH from 6 to 7 is added to the gel phase. The mixture is then transferred to a high speed vacuum mixer. ; where Sylodent® XWA 650, Sylodent® 783 abrasive silica is added, and

10 silica thickener ZEODENT® 165. The mixture is then mixed at high speed for 5 to 30 minutes, under a vacuum of about 20 to 50 mm Hg, preferably about 30 mm Hg. The aromatic oil and oregano extract are added and then mixed. Finally, surfactants, such as sodium lauryl sulfate (SLS), are added to the mixer. The resulting product is a gel or paste product, semi-solid, extrudable.

TABLE I Ingredient

Final Weight %

Oregano Extract

0.3

TSPP

 1.0

STPP

 7.0

GANTREZ ® S97 liquid solution

1.0

Sorbitol

18.7

Glycerin

 12.0

Sodium fluoride

0.243

Sodium sacharine

0.3

Sodium hydroxide

1.0

CMC 2000S

0.8

Carrageenan

0.4

Sylodent ® 783

11.0

Sylodent ® XWA 650

10.0

ZEODENT ® 165

3.5

Sodium lauryl sulfate

1.2

Mica coated with TiO2

 0.1

Aroma (89-332)

1.0

Blue solution

0.05

Water

C.S.

Claims (12)

one.

 An oral care composition in the form of a dentifrice comprising an active ingredient comprising a safe and effective amount of one or more active compounds of an oregano extract, wherein at least one of the one or more active compounds of the oregano extract is selects between carvacrol, thymol and rosmarinic acid, an anti-tartar system comprising as active ingredients to control tartar from 0.5 to 1.5% by weight of tetrasodium pyrophosphate, from 1 to 10% by weight of sodium tripolyphosphate and 0.5 to 1.5% by weight of a copolymer of maleic anhydride and methyl vinyl ether, amounts in weight% based on the weight of the composition, and an orally acceptable carrier.

2.

 An oral care composition according to claim 1, wherein the active ingredient comprises an oregano extract.

3.

 An oral care composition according to claim 1, wherein the active ingredient consists essentially of one or more active compounds of an oregano extract.

Four.

 An oral care composition according to claim 1, wherein the active ingredient consists essentially of an oregano extract.

5.

 An oral composition according to claim 1, wherein the active ingredient is present in the oral care composition at a concentration of 0.001 to 10% by weight.

6.

 An oral composition according to claim 1, wherein the active ingredient is present in the oral composition at a concentration of 0.01 to 5% by weight.

7.

 An oral composition according to claim 1, wherein the active ingredient is present in the oral composition at a concentration of 0.01 to 3% by weight.

8.

 An oral composition according to claim 1, wherein the oral composition further comprises an additional active ingredient.

9.

 An oral composition according to claim 8, wherein the additional active ingredient is selected from the group of: antibacterial agents, antioxidants, vitamins, minerals, nutrients, hydrating agents of the mouth, sialagoges, emollients, anticaries agents, desensitizing agents, anti agents -inflammatory agents, antiplatelet agents, anti-halitosis agents, and combinations thereof.

10.

 An oral composition according to claim 8, wherein the additional active ingredient is selected from the group consisting of: 2,4,4'-trichloro-2'-hydroxy diphenyl ether (triclosan), stannous fluoride, zinc citrate, potassium nitrate , sodium metaphosphate, and combinations thereof.

eleven.

 An oral composition according to claim 1, wherein the oral composition further comprises 2,4,4'-trichloro-2'-hydroxy diphenyl ether (triclosan).

12.

 An oral composition according to claim 1, wherein the orally acceptable carrier comprises one or more oral care ingredients selected from the group consisting of: viscosity modifiers, diluents, surfactants, pH modifying agents, abrasives, moisturizers, agents to impart sensation in the mouth, sweetening agents, flavoring agents, colorants, preservatives, vitamins, compatible enzymes, chlorophyll compounds and combinations thereof.